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Assay Detail

CHEMBL656554

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Inhibition of human CX3C chemokine receptor 5 from GP120-membrane-based assay
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Expert

Target

C-C chemokine receptor type 5 (CHEMBL274)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Antagonists of human CCR5 receptor containing 4-(pyrazolyl)piperidine side chains. Part 1: Discovery and SAR study of 4-pyrazolylpiperidine side chains.
Shen DM, Shu M, Mills SG, Chapman KT, Malkowitz L, Springer MS, Gould SL, DeMartino JA, Siciliano SJ, Kwei GY, Carella A, Carver G, Holmes K, Schleif WA, Danzeisen R, Hazuda D, Kessler J, Lineberger J, Miller MD, Emini EA.
Bioorg Med Chem Lett (2004) 14 : 935 -939
PubMed 15012997 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 13 8.41 9.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL102826 1 9.70
CHEMBL367837 1 9.22
CHEMBL368183 1 9.00
CHEMBL367838 1 8.66
CHEMBL81252 1 8.62
CHEMBL174303 1 8.40
CHEMBL367446 1 8.12
CHEMBL366439 1 8.12
CHEMBL369189 1 8.05
CHEMBL170717 1 8.05
CHEMBL435526 1 7.92
CHEMBL172944 1 7.80
CHEMBL172721 1 7.64

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL102826 IC50 = 0.2 nM 9.70
CHEMBL367837 IC50 = 0.6 nM 9.22
CHEMBL368183 IC50 = 1.0 nM 9.00
CHEMBL367838 IC50 = 2.2 nM 8.66
CHEMBL81252 IC50 = 2.4 nM 8.62
CHEMBL174303 IC50 = 4.0 nM 8.40
CHEMBL367446 IC50 = 7.5 nM 8.12
CHEMBL366439 IC50 = 7.5 nM 8.12
CHEMBL369189 IC50 = 9.0 nM 8.05
CHEMBL170717 IC50 = 9.0 nM 8.05
CHEMBL435526 IC50 = 12.0 nM 7.92
CHEMBL172944 IC50 = 16.0 nM 7.80
CHEMBL172721 IC50 = 23.0 nM 7.64